Hollow pessary loaded with lawsone via self-microemulsifying drug delivery system for vaginal candidiasis

• Published in: Journal of drug delivery science and technology 2020-12, Vol.60, p.101955, Article 101955
• Main Authors: Pandit, Ashlesha, Kedar, Ashwini, Koyate, Kanchan
• Format: Article
• Language: English
• Subjects: Gelucire 44/14; Lawsone; Ovucire WL 3460; SMEDDS; Vaginal candidiasis
• ISSN: 1773-2247
• DOI: 10.1016/j.jddst.2020.101955

An attempt was made to enhance solubility of an antifungal agent lawsone, via self-microemulsifying drug delivery system (SMEDDS), formulated further into hollow pessary to treat vaginal candidiasis. Microemulsion was formed at 20% capryol 90® (oil); 80% Gelucire 44/14® (surfactant) and 20% Tween 80 (co-surfactant), which was plotted using pseudo-ternary phase diagram using aqueous titration method. Zeta potential −10.9 ± 0.54 mV and particle size 12.19 ± 1.13 nm confirmed the formation of microemulsion. Quick self-emulsification time (55 s) indicated rapid emulsification process at vaginal site. Cloud point confirmed the stability of SMEDDS (up to 60 °C). Lawsone-loaded SMEDDS exhibited improved solubility of lawsone (216 ± 2.54 mg/ml and 0.542 ± 0.04 mg/ml, respectively) and dissolution, which further helped to enhance its antifungal activity. Pessary base, consisted of Ovucire WL3460® (94, 96, 98) and beeswax (2, 4, 6), was optimized using three-level, two-factor full factorial design. Hollow pessary was further fabricated using melted base (at 60 °C), which was poured into aluminum mold fitted with center tube. This center tube was filled with lawsone-loaded SMEDDS and was solidified at 2–8 °C. Pessary was melted within 7 ± 1.1 min at 37 °C and released 96.96 ± 1.43% lawsone within 1 h at simulated vaginal fluid. Lawsone SMEDDS loaded pessary released lawsone at par with marketed clotrimazole vaginal tablet. To conclude, hollow pessary of lawsone-loaded SMEDDS can be an advanced modality to treat vulvo-vaginal candidiasis. [Display omitted]